Global Patent Index - EP 2054389 A1

EP 2054389 A1 20090506 - 6-SUBSTITUTED ISOQUINOLINE DERIVATIVES AS ROCK-1 INHIBITORS

Title (en)

6-SUBSTITUTED ISOQUINOLINE DERIVATIVES AS ROCK-1 INHIBITORS

Title (de)

6-SUBSTITUIERTE ISOCHINOLINDERIVATE ALS ROCK-1-INHIBITOREN

Title (fr)

DÉRIVÉS D'ISOQUINOLÉINE SUBSTITUÉS EN POSITION 6 EN TANT QU'INHIBITEURS DE ROCK-1

Publication

EP 2054389 A1 20090506 (EN)

Application

EP 07802697 A 20070817

Priority

  • EP 2007058593 W 20070817
  • EP 06119142 A 20060818
  • EP 07802697 A 20070817

Abstract (en)

[origin: WO2008020081A1] The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH<SUB>2</SUB>; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R<SUB>1</SUB> is H, when Y is NH<SUB>2</SUB>; or R<SUB>1</SUB> is H, (C<SUB>1-4</SUB>)alk yl or halogen, when Y is OH; R<SUB>2</SUB> and R<SUB>3</SUB> are independently H, (C<SUB>1-4</SUB>)alkyl or halogen; R<SUB>4</SUB> is H or (C<SUB>1-6</SUB>)alkyl, optionally substituted with halogen, (C<SUB>3-7</SUB>)cycloalkyl, (C<SUB>6-10</SUB>)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C<SUB>6-10</SUB>)aryl and heterocyclic ring being optionally substituted with (C<SUB>1-4</SUB>)alkyl, (C<SUB>1-4</SUB>)alkyloxy or halogen; R<SUB>5</SUB> is H or (C<SUB>1-4</SUB>)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH, n is 0 and m+o =2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.

IPC 8 full level

C07D 217/22 (2006.01); A61K 31/472 (2006.01); A61P 9/10 (2006.01); A61P 27/06 (2006.01); C07D 217/24 (2006.01)

CPC (source: EP US)

A61P 9/10 (2017.12 - EP); A61P 9/12 (2017.12 - EP); A61P 27/06 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 217/22 (2013.01 - EP US); C07D 217/24 (2013.01 - EP US)

Citation (search report)

See references of WO 2008020081A1

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE SI SK TR

Designated extension state (EPC)

AL BA HR MK RS

DOCDB simple family (publication)

WO 2008020081 A1 20080221; AT E463483 T1 20100415; CA 2660489 A1 20080221; CN 101522633 A 20090902; CN 101522633 B 20120509; DE 602007005811 D1 20100520; EP 2054389 A1 20090506; EP 2054389 B1 20100407; ES 2341809 T3 20100628; JP 2010501480 A 20100121; JP 5341758 B2 20131113; MX 2009001804 A 20090226; US 2008045566 A1 20080221; US 7893088 B2 20110222

DOCDB simple family (application)

EP 2007058593 W 20070817; AT 07802697 T 20070817; CA 2660489 A 20070817; CN 200780036804 A 20070817; DE 602007005811 T 20070817; EP 07802697 A 20070817; ES 07802697 T 20070817; JP 2009524205 A 20070817; MX 2009001804 A 20070817; US 83970307 A 20070816